Abstract: Citri Fructus is a well-known traditional Chinese medicine with surely curative efficacy on regulating the Qi, which has been widely applied in clinical treatments. In this paper, the research advances of Citri Fructus on chemical constituents and pharmacological effects were comprehensively summarized. There were 167 kinds of compounds which have been reported, including volatile oils, flavonoids, coumarins, alkaloids and terpenes. Citri Fructus has good pharmacological activity in anti-oxidation, anti-inflammatory, anti-allergic, anti-bacterial, anti-tumor. The concept of quality marker was introduced and a predictive analysis of Citri Fructus about quality marker was performed in terms of component specificity, constituent validity and component measurability. It is suggested that dipentene, citral, naringin, hesperidin and limonin and compounds in Citrus wilsonii Tanaka(linalool, α-pinene, β-pinene, terpinyl propionate and osthole), as well as two compounds isolated from Citrus medica L. (nobiletin, synephrine) were considered as quality markers. This paper not only provided a theoretical basis for the establishment of quality control standard, but promoted in-depth research and utilization of Citri Fructus.